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Drug Strategies Targeting CYP51 in Neglected Tropical Diseases

Chemical reviews, 2014-11, Vol.114 (22), p.11242-11271

2014

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Enzymatic chokepoints and synergistic drug targets in the sterol biosynthesis pathway of Naegleria fowleri

PLoS pathogens, 2018-09, Vol.14 (9), p.e1007245

2018

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Enzymatic hydroxylation of an unactivated methylene C-H bond guided by molecular dynamics simulations

Nature chemistry, 2015-08, Vol.7 (8), p.653-660

2015

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X-ray structures of thioredoxin and thioredoxin reductase from Entamoeba histolytica and prevailing hypothesis of the mechanism of Auranofin action

Journal of structural biology, 2016-05, Vol.194 (2), p.180-190

2016

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CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)

PLoS neglected tropical diseases, 2017-12, Vol.11 (12), p.e0006104

2017

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New Reactions and Products Resulting from Alternative Interactions between the P450 Enzyme and Redox Partners

Journal of the American Chemical Society, 2014-03, Vol.136 (9), p.3640-3646

2014

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Solution Conformations and Dynamics of Substrate-Bound Cytochrome P450 MycG

Biochemistry (Easton), 2017-05, Vol.56 (21), p.2701-2714

2017

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Directing Group-Controlled Regioselectivity in an Enzymatic C–H Bond Oxygenation

Journal of the American Chemical Society, 2014-04, Vol.136 (13), p.4901-4904

2014

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Structural characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei bound to the antifungal drugs posaconazole and fluconazole

PLoS neglected tropical diseases, 2010-04, Vol.4 (4), p.e651

2010

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Engineering and Analysis of a Self-Sufficient Biosynthetic Cytochrome P450 PikC Fused to the RhFRED Reductase Domain

Journal of the American Chemical Society, 2007-10, Vol.129 (43), p.12940-12941

2007

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Selective Oxidation of Carbolide C-H Bonds by an Engineered Macrolide P450 Mono-Oxygenase

Proceedings of the National Academy of Sciences - PNAS, 2009-11, Vol.106 (44), p.18463-18468

2009

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Substrate Recognition by the Multifunctional Cytochrome P450 MycG in Mycinamicin Hydroxylation and Epoxidation Reactions

The Journal of biological chemistry, 2012-11, Vol.287 (45), p.37880-37890

2012

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Tirandamycin biosynthesis is mediated by co-dependent oxidative enzymes

Nature chemistry, 2011-07, Vol.3 (8), p.628-633

2011

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4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection

PLoS neglected tropical diseases, 2017-12, Vol.11 (12), p.e0006132

2017

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Biochemical and structural characterization of CYP124: A methyl-branched lipid ω-hydroxylase from Mycobacterium tuberculosis

Proceedings of the National Academy of Sciences - PNAS, 2009-12, Vol.106 (49), p.20687-20692

2009

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A highly conserved mycobacterial cholesterol catabolic pathway

Environmental microbiology, 2013-08, Vol.15 (8), p.2342-2359

2013

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Diversity of P450 enzymes in the biosynthesis of natural products

Natural product reports, 2012-01, Vol.29 (10), p.1251-1266

2012

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The Schistosoma mansoni Cytochrome P450 (CYP3050A1) Is Essential for Worm Survival and Egg Development

PLoS neglected tropical diseases, 2015-12, Vol.9 (12), p.e0004279-e0004279

2015

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2.3 Å X-ray Structure of the Heme-Bound GAF Domain of Sensory Histidine Kinase DosT of Mycobacterium tuberculosis

Biochemistry (Easton), 2008-11, Vol.47 (47), p.12523-12531

2008

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The Structural Basis for Substrate Anchoring, Active Site Selectivity, and Product Formation by P450 PikC from Streptomyces venezuelae

The Journal of biological chemistry, 2006-09, Vol.281 (36), p.26289-26297

2006

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Analysis of Transient and Catalytic Desosamine-binding Pockets in Cytochrome P-450 PikC from Streptomyces venezuelae

The Journal of biological chemistry, 2009-02, Vol.284 (9), p.5723-5730

2009

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Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51

PLoS neglected tropical diseases, 2012-07, Vol.6 (7), p.e1736-e1736

2012

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Homodimerization Counteracts the Detrimental Effect of Nitrogenous Heme Ligands on the Enzymatic Activity of Acanthamoeba castellanii CYP51

Biochemistry (Easton), 2022-07, Vol.61 (13), p.1363-1377

2022

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The Antifungal Drug Isavuconazole Is both Amebicidal and Cysticidal against Acanthamoeba castellanii

Antimicrobial agents and chemotherapy, 2020-04, Vol.64 (5)

2020

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Dynamic visualization of type II peptidyl carrier protein recognition in pyoluteorin biosynthesis

RSC chemical biology, 2020-04, Vol.1 (1), p.8-12

2020

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Drug Strategies Targeting CYP51 in Neglected Tropical Diseases

Enzymatic chokepoints and synergistic drug targets in the sterol biosynthesis pathway of Naegleria fowleri

Enzymatic hydroxylation of an unactivated methylene C-H bond guided by molecular dynamics simulations

X-ray structures of thioredoxin and thioredoxin reductase from Entamoeba histolytica and prevailing hypothesis of the mechanism of Auranofin action

CYP51 is an essential drug target for the treatment of primary amoebic meningoencephalitis (PAM)

New Reactions and Products Resulting from Alternative Interactions between the P450 Enzyme and Redox Partners

Solution Conformations and Dynamics of Substrate-Bound Cytochrome P450 MycG

Directing Group-Controlled Regioselectivity in an Enzymatic C–H Bond Oxygenation

Structural characterization of CYP51 from Trypanosoma cruzi and Trypanosoma brucei bound to the antifungal drugs posaconazole and fluconazole

Engineering and Analysis of a Self-Sufficient Biosynthetic Cytochrome P450 PikC Fused to the RhFRED Reductase Domain

Selective Oxidation of Carbolide C-H Bonds by an Engineered Macrolide P450 Mono-Oxygenase

Substrate Recognition by the Multifunctional Cytochrome P450 MycG in Mycinamicin Hydroxylation and Epoxidation Reactions

Tirandamycin biosynthesis is mediated by co-dependent oxidative enzymes

4-aminopyridyl-based lead compounds targeting CYP51 prevent spontaneous parasite relapse in a chronic model and improve cardiac pathology in an acute model of Trypanosoma cruzi infection

Biochemical and structural characterization of CYP124: A methyl-branched lipid ω-hydroxylase from Mycobacterium tuberculosis

A highly conserved mycobacterial cholesterol catabolic pathway

Diversity of P450 enzymes in the biosynthesis of natural products

The Schistosoma mansoni Cytochrome P450 (CYP3050A1) Is Essential for Worm Survival and Egg Development

2.3 Å X-ray Structure of the Heme-Bound GAF Domain of Sensory Histidine Kinase DosT of Mycobacterium tuberculosis

The Structural Basis for Substrate Anchoring, Active Site Selectivity, and Product Formation by P450 PikC from Streptomyces venezuelae

Analysis of Transient and Catalytic Desosamine-binding Pockets in Cytochrome P-450 PikC from Streptomyces venezuelae

Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51

Homodimerization Counteracts the Detrimental Effect of Nitrogenous Heme Ligands on the Enzymatic Activity of Acanthamoeba castellanii CYP51

The Antifungal Drug Isavuconazole Is both Amebicidal and Cysticidal against Acanthamoeba castellanii

Dynamic visualization of type II peptidyl carrier protein recognition in pyoluteorin biosynthesis

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